Kinetic modelling of liposome degradation in serum: Effect of size and concentration of liposomes in vitro

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Abstract
The purpose of this study is to propose a new method for quantitative evaluation of liposome degradation in serum. The time course of liposome degradation in rat serum was monitored continuously, using 6(5)-carboxyfluorescein as an aqueous phase marker. The degradation curves exhibited three characteristic phases: lag time, degradation, and plateau. This curve was described by a kinetic model with three parameters: lag time (τ), first-order degradation rate constant (k), and maximum degradation (α). The rate and extent of the degradation of liposomes were evaluated separately in terms of k and α, respectively. The effects of size and concentration of liposomes on their degradation kinetics were examined using this method. Both k and α increased with increasing liposomal size. The increased affinity of larger liposomes for complement was suggested to increase both k and α. On the other hand, α decreased with increasing liposomal concentration without altering k. The decreased extent of degradation was considered to result from the depletion of complement components. There was no significant effect of size and concentration of liposomes on τ. Quantitative evaluation of the rate and extent of degradation of liposomes will provide deeper insights into the interaction between liposomes and serum components, and basic information on liposomes as potential drug carriers.

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